Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
This is a single-center, open-label, randomized, two-stage, two-way crossover Phase I study in healthy male subjects.The main objective is to evaluate the differences in pharmadynamics (PD), pharmacokinetics (PK), and safety between ciprofol injectable emulsion and propofol injectable emulsion at different doses in healthy subjects.
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Ciprofol | Experimental | First-stage: 0.4mg/kg, 0.6 mg/kg, 0.8 mg/kg Second-stage: 0.4mg/kg, 0.6 mg/kg, 0.8 mg/kg |
|
| Propofol | Active Comparator | First-stage: 2.0mg/kg, 3.0 mg/kg, 4.0 mg/kg Second-stage: 2.0mg/kg, 3.0 mg/kg, 4.0 mg/kg |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Ciprofol | Drug | First-stage: 0.4mg/kg, 0.6 mg/kg, 0.8 mg/kg Second-stage: 0.4mg/kg, 0.6 mg/kg, 0.8 mg/kg |
|
| Measure | Description | Time Frame |
|---|---|---|
| Modified observer's assessment of alertness/sedation(MOAA/S) | Observe the change of modified observer's assessment of alert /sedation during the whole trial | From first dose of study drug until fully alert on day 1 |
| Bispectral index (BIS) | From first dose of study drug until fully alert on day 1 | |
| Safety by measurement of Adverse Events | First dose of study drug on day 1 |
| Measure | Description | Time Frame |
|---|---|---|
| Peak concentration (Cmax) | First dose of study drug on day 1 | |
| Area under the plasma concentration versus time curve (AUC) | First dose of study drug on day 1 | |
| Measure | Description | Time Frame |
|---|---|---|
| Use of dynamometer to estimate Muscular strength of lower limbs | From 30 minutes before administration to 1 hour after administration on day 1 | |
| The differences between the Montreal Cognitive Assessment (MoCA) test score in Ciprofol group and in a control group of Propofol |
Inclusion Criteria:
Exclusion Criteria:
Patients with known allergies to ciprofol injectable emulsion, excipient in propofol injectable emulsion (soybean oil, glycerin, triglyceride, egg lecithin, sodium oleate, and sodium hydroxide); history of drug allergies (including other anesthetics), allergic diseases, or hyperactive immune response;
Patients receiving any of the following drugs or therapies prior to screening/administration:
Patients with history or evidence of any of the following diseases prior to screening/administration:
Laboratory results meeting any of the following during screening/at baseline:
ALT or AST > 50% of ULN; Creatinine > 20% of ULN; Total bilirubin > 40% of ULN.
History of alcohol abuse within 3 months prior to screening; alcohol abuse defined as average of > 2 units of alcohol per day (1 unit = 360 mL beer or 45 mL liquor with 40% alcohol or 150 mL wine), or positive alcohol breath test results at baseline;
Patients who smoked more than 5 cigarettes per day and a total of more than 60 cigarettes within 3 months prior to screening;
Blood donation or blood loss ≥ 200 mL within 30 days prior to screening; plasma donation or plasma exchange within 7 days prior to screening;
Subjects who consumed any beverages or foods containing alcohol, grapefruit juice or methylxanthine (such as coffee, tea, cola, chocolate, and energy drinks), participated in strenuous physical activities and had other factors that may affect drug absorption, distribution, metabolism, and excretion, within 2 days prior to baseline; subjects who were unable to fast for 8 hours before dose administration;
Subjects who were expected to go through surgery or hospitalization during the trial;
Subjects unsuitable for arterial blood collection, such as subjects with positive results in Allen's test;
Subjects who were unwilling to practice contraception during the trial; subjects who were planning to conceive within 3 month after the completion of the trial;
Subjects judged by the investigators to be unsuitable for participating in this trial for any reason.
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Sichuan Provincial People's Hospital | Chengdu | China |
Not provided
| ID | Term |
|---|---|
| C000730795 | (2-(1R)-1-cyclopropyl)ethyl-6-isopropyl-phenol |
| D015742 | Propofol |
| ID | Term |
|---|---|
| D010636 | Phenols |
| D001555 | Benzene Derivatives |
| D006841 | Hydrocarbons, Aromatic |
| D006844 | Hydrocarbons, Cyclic |
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
Not provided
| Propofol | Drug | First-stage: 2.0mg/kg, 3.0 mg/kg, 4.0 mg/kg Second-stage: 2.0mg/kg, 3.0 mg/kg, 4.0 mg/kg |
|
| Terminal half-life (t1/2) |
| First dose of study drug on day 1 |
| time to peak concentration (Tmax) | First dose of study drug on day 1 |
| clearance (CL) | First dose of study drug on day 1 |
| mean residence time (MRT) | First dose of study drug on day 1 |
| volume of distribution (Vz) | First dose of study drug on day 1 |
Total score of the MoCA,the higher scores mean a better outcome
| From the baseline period to 1 hour after administration on day 1 |
| D006838 |
| Hydrocarbons |
| D009930 | Organic Chemicals |